Icilin (AG-3-5) is a super-agonist of the transient receptor potential M8 (TRPM8) ion channel. Icilin activates TRPM8 in EGTA in a dose-dependent manner (EC50=1.4 μM). Icilin is a “super-cooling agent”. Icilin attenuates autoimmune neuroinflammation through modulation of the T-cell response
靶点:
TRPM8
体内研究:
Icilin is a transient receptor potential cation channel subfamily M (TRPM8) agonist that produces behavioral activation in rats and mice. Icilin (3 mg/kg; s.c.) induces“Wet dog shake” in mice
参考文献:
1. Huai-hu Chuang, et al. The super-cooling agent icilin reveals a mechanism of coincidence detection by a temperature-sensitive TRP channel. Neuron. 2004 Sep 16;43(6):859-69. 2. Viktor V Feketa,et al. Transient receptor potential melastatin 8 channel inhibition potentiates the hypothermic response to transient receptor potential vanilloid 1 activation in the conscious mouse. Crit Care Med. 2014 May;42(5):e355-63. 3. Benjamin W Ewanchuk, et al. The cooling compound icilin attenuates autoimmune neuroinflammation through modulation of the T-cell response. FASEB J. 2018 Mar;32(3):1236-1249.